title: Synthetic chalcones as efficient inhibitors of Mycobacterium tuberculosis protein tyrosine phosphatase PtpA.
abstract: In the search for lead compounds for new drugs for tuberculosis, the activity of 38 synthetic chalcones were assayed for their potential inhibitory action towards a protein tyrosine phosphatase from Mycobacterium tuberculosis--PtpA. The compounds were obtained by aldolic condensation between aldehydes and acetophenones, under basic conditions. Five compounds presented moderate or good activity. The structure-activity analysis reveals that the predominant factor for the activity is the molecule planarity/hydrophobicity and the nature of the substituents.
authors.affiliation: Departamento de Química, Universidade Federal de Santa Catarina, Campus Trindade, 88040-900 Florianópolis, SC, Brazil.
authors.forename: Louise Domeneghini
authors.initials: LD
authors.lastname: Chiaradia
authors.forename: Alessandra
authors.initials: A
authors.lastname: Mascarello
authors.forename: Marcela
authors.initials: M
authors.lastname: Purificação
authors.forename: Javier
authors.initials: J
authors.lastname: Vernal
authors.forename: Marlon Norberto Sechini
authors.initials: MN
authors.lastname: Cordeiro
authors.forename: María Emilia
authors.initials: ME
authors.lastname: Zenteno
authors.forename: Andréa
authors.initials: A
authors.lastname: Villarino
authors.forename: Ricardo José
authors.initials: RJ
authors.lastname: Nunes
authors.forename: Rosendo Augusto
authors.initials: RA
authors.lastname: Yunes
authors.forename: Hernán
authors.initials: H
authors.lastname: Terenzi
mesh_terms: D001426:Bacterial Proteins; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D024881:Drug Resistance, Bacterial / Q000187:drug effects; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000201:enzymology*; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors* / Q000235:genetics; D013329:Structure-Activity Relationship; D014376:Tuberculosis / Q000188:drug therapy
chemical_list: D001426:Bacterial Proteins; D047188:Chalcones; C414465:MptpA protein, Mycobacterium tuberculosis; D017027:Protein Tyrosine Phosphatases